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Effects of absorption enhancers on the transport of model compounds in Caco-2 cell monolayers: assessment by confocal laser scanning microscopy.
J Pharm Sci. 1997 Jul; 86(7):779-85.JP

Abstract

Three typical absorption enhancers, i.e., sodium caprate (Cap-Na), sodium deoxycholate (Deo-Na), and dipotassium glycyrrhizinate (Grz-K), were compared in terms of their permeability-enhancing effects on hydrophilic and hydrophobic model compounds in Caco-2 cell monolayers. The transepithelial electrical resistance (TEER) of the monolayers was reduced concentration-dependently by treatment with Cap-Na and Deo-Na, while treatment with Grz-K increased the TEER. Two patterns of TEER reduction were observed: one pattern indicated that Cap-Na had a rapid reducing effect, and another indicated that Deo-Na had a delayed reducing effect. These reductions in the TEER were accompanied by the increased transepithelial transport of two hydrophilic model compounds, sodium fluorescein (Flu-Na; MW = 376, log P = -1.52) and fluorescein isothiocyanate-dextran 4000 (FD-4; MW = 4400, log P = -2.0), and one hydrophobic model compound, rhodamine 123 hydrate (Rh123; MW = 381, log P = 1.13). The transport-enhancing effects of Cap-Na and Deo-Na on these model compounds decreased in the following order: FD-4 > Rh123 > Flu-Na, while Grz-K was found to have no effect on the transport of any of these model compounds. Confocal laser scanning microscopy (CLSM) of Caco-2 cell monolayers revealed that Cap-Na and Deo-Na enhanced the transepithelial transport of the hydrophilic model compounds via the paracellular route and that of the hydrophobic model compound via both paracellular and transcellular routes. Semiquantitative visual information obtained from CLSM images reflected the results of the transport experiment.

Authors+Show Affiliations

Tsukuba Laboratories, Hisamitsu Pharmaceutical Company, Inc., Ibaraki, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

9232516

Citation

Sakai, M, et al. "Effects of Absorption Enhancers On the Transport of Model Compounds in Caco-2 Cell Monolayers: Assessment By Confocal Laser Scanning Microscopy." Journal of Pharmaceutical Sciences, vol. 86, no. 7, 1997, pp. 779-85.
Sakai M, Imai T, Ohtake H, et al. Effects of absorption enhancers on the transport of model compounds in Caco-2 cell monolayers: assessment by confocal laser scanning microscopy. J Pharm Sci. 1997;86(7):779-85.
Sakai, M., Imai, T., Ohtake, H., Azuma, H., & Otagiri, M. (1997). Effects of absorption enhancers on the transport of model compounds in Caco-2 cell monolayers: assessment by confocal laser scanning microscopy. Journal of Pharmaceutical Sciences, 86(7), 779-85.
Sakai M, et al. Effects of Absorption Enhancers On the Transport of Model Compounds in Caco-2 Cell Monolayers: Assessment By Confocal Laser Scanning Microscopy. J Pharm Sci. 1997;86(7):779-85. PubMed PMID: 9232516.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of absorption enhancers on the transport of model compounds in Caco-2 cell monolayers: assessment by confocal laser scanning microscopy. AU - Sakai,M, AU - Imai,T, AU - Ohtake,H, AU - Azuma,H, AU - Otagiri,M, PY - 1997/7/1/pubmed PY - 2000/7/19/medline PY - 1997/7/1/entrez SP - 779 EP - 85 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 86 IS - 7 N2 - Three typical absorption enhancers, i.e., sodium caprate (Cap-Na), sodium deoxycholate (Deo-Na), and dipotassium glycyrrhizinate (Grz-K), were compared in terms of their permeability-enhancing effects on hydrophilic and hydrophobic model compounds in Caco-2 cell monolayers. The transepithelial electrical resistance (TEER) of the monolayers was reduced concentration-dependently by treatment with Cap-Na and Deo-Na, while treatment with Grz-K increased the TEER. Two patterns of TEER reduction were observed: one pattern indicated that Cap-Na had a rapid reducing effect, and another indicated that Deo-Na had a delayed reducing effect. These reductions in the TEER were accompanied by the increased transepithelial transport of two hydrophilic model compounds, sodium fluorescein (Flu-Na; MW = 376, log P = -1.52) and fluorescein isothiocyanate-dextran 4000 (FD-4; MW = 4400, log P = -2.0), and one hydrophobic model compound, rhodamine 123 hydrate (Rh123; MW = 381, log P = 1.13). The transport-enhancing effects of Cap-Na and Deo-Na on these model compounds decreased in the following order: FD-4 > Rh123 > Flu-Na, while Grz-K was found to have no effect on the transport of any of these model compounds. Confocal laser scanning microscopy (CLSM) of Caco-2 cell monolayers revealed that Cap-Na and Deo-Na enhanced the transepithelial transport of the hydrophilic model compounds via the paracellular route and that of the hydrophobic model compound via both paracellular and transcellular routes. Semiquantitative visual information obtained from CLSM images reflected the results of the transport experiment. SN - 0022-3549 UR - https://www.unboundmedicine.com/medline/citation/9232516/Effects_of_absorption_enhancers_on_the_transport_of_model_compounds_in_Caco_2_cell_monolayers:_assessment_by_confocal_laser_scanning_microscopy_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)50350-X DB - PRIME DP - Unbound Medicine ER -